Shabatina Tatyana I, Gromova Yana A, Vernaya Olga I, Soloviev Andrei V, Shabatin Andrei V, Morosov Yurii N, Astashova Irina V, Melnikov Michail Y
Department of Chemistry, M.V. Lomonosov Moscow State University, Moscow 119991, Russia.
Faculty of Fundamental Sciences, N.E. Bauman Moscow Technical State University, Moscow 105005, Russia.
Pharmaceuticals (Basel). 2024 May 5;17(5):587. doi: 10.3390/ph17050587.
The use of medicinal substances in nanosized forms (nanoforms, nanoparticles) allows the therapeutic effectiveness of pharmaceutical preparations to be increased due to several factors: (1) the high specific surface area of nanomaterials, and (2) the high concentration of surface-active centers interacting with biological objects. In the case of drug nanoforms, even low concentrations of a bioactive substance can have a significant therapeutic effect on living organisms. These effects allow pharmacists to use lower doses of active components, consequently lowering the toxic side effects of pharmaceutical nanoform preparations. It is known that many drug substances that are currently in development are poorly soluble in water, so they have insufficient bioavailability. Converting them into nanoforms will increase their rate of dissolution, and the increased saturation solubility of drug nanocrystals also makes a significant contribution to their high therapeutic efficiency. Some physical and chemical methods can contribute to the formation of both pure drug nanoparticles and their ligand or of polymer-covered nanoforms, which are characterized by higher stability. This review describes the most commonly used methods for the preparation of nanoforms (nanoparticles) of different medicinal substances, paying close attention to modern supercritical and cryogenic technologies and the advantages and disadvantages of the described methods and techniques; moreover, the improvements in the physico-chemical and biomedical properties of the obtained medicinal nanoforms are also discussed.
使用纳米尺寸形式（纳米形式、纳米颗粒）的药用物质可因多种因素提高药物制剂的治疗效果：（1）纳米材料的高比表面积，以及（2）与生物物体相互作用的高浓度表面活性中心。就药物纳米形式而言，即使低浓度的生物活性物质也可对生物体产生显著的治疗效果。这些效果使药剂师能够使用更低剂量的活性成分，从而降低药物纳米形式制剂的毒副作用。众所周知，许多目前正在研发的药物物质在水中的溶解度很差，因此它们的生物利用度不足。将它们转化为纳米形式将提高其溶解速率，并且药物纳米晶体增加的饱和溶解度也对其高治疗效率做出了重大贡献。一些物理和化学方法有助于形成纯药物纳米颗粒及其配体或聚合物包覆的纳米形式，其特点是具有更高的稳定性。本综述描述了制备不同药用物质的纳米形式（纳米颗粒）最常用的方法，密切关注现代超临界和低温技术以及所描述方法和技术的优缺点；此外，还讨论了所得药用纳米形式的物理化学和生物医学性质的改善情况。
